Synthesis and pharmacological activity of acetylenic piperidinediols

…, AM Zvonok, AP Lugovskii, LA Melentovich…

Index: Zakharevskii, A. S.; Zvonok, A. M.; Lugovskii, A. P.; Melentovich, L. A.; Stanishevskii, L. S.; Yushkevich, E. V. Pharmaceutical Chemistry Journal, 1989 , vol. 23, # 2 p. 140 - 143 Khimiko-Farmatsevticheskii Zhurnal, 1989 , vol. 23, # 2 p. 178 - 182

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Abstract

It was found that reaction of sodium acetylide with piperidones (X-XVI) in liquid ammonia resulted in the preferential formation of 3e, 4e-dihydroxy-6e-aryl-l, 3a-dimethyl-4a- ethynylpiperidines (XIX-XXV), the ratio of 3e, 4e-to 3e, 4a-diols, as found by preparative column chromatography on alumina, being 4: 1-7: 1. When ethynylmagnesium bromide was used, in addition to the 3e, 4e-diols there were also obtained the 6e-aryl-3e, 4a- ...